RU93005332A - DERIVATIVES 4,1-BENZOXAZEPINA, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT - Google Patents
DERIVATIVES 4,1-BENZOXAZEPINA, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENTInfo
- Publication number
- RU93005332A RU93005332A RU93005332/04A RU93005332A RU93005332A RU 93005332 A RU93005332 A RU 93005332A RU 93005332/04 A RU93005332/04 A RU 93005332/04A RU 93005332 A RU93005332 A RU 93005332A RU 93005332 A RU93005332 A RU 93005332A
- Authority
- RU
- Russia
- Prior art keywords
- optionally substituted
- hydrogen atom
- derivatives
- benzoxazepina
- treatment
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- VTYJANRVLSSNCJ-UHFFFAOYSA-N 4,1-benzoxazepin-2-one Chemical class O=C1COC=C2C=CC=CC2=N1 VTYJANRVLSSNCJ-UHFFFAOYSA-N 0.000 claims 1
- 108010022535 Farnesyl-Diphosphate Farnesyltransferase Proteins 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000004429 atoms Chemical group 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 230000002538 fungal Effects 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
Claims (1)
где R1 является атомом водорода или необязательно замещенной углеводородной группой; R2 и R3 независимо являются атомом водорода, необязательно замещенным низшим алкилом, необязательно замещенным фенилом или необязательно замещенной ароматической гетероциклической группой; X является связью или спейсером, имеющим длину цепи от 1 до 7 атомов; Y является необязательно этерифицированным или тиоэтерифицированным карбоксилом, необязательно замещенным гидроксилом, необязательно замещенной аминогруппой, необязательно замещенным фенилом, необязательно замещенным карбамоилом или N - содержащим гетероциклическим остатком, имеющим атом водорода, способный быть депротонированным; при условии, что когда X является метиленом и R1 не является алкилом, содержащим больше 4 атомов углерода, Y не является ни карбоксилом, ни алкоксикарбонилом; кольцо A может быть необязательно замещенным, или его соли, которые являются полезными для ингибирования скваленсинтетазы и роста грибов.Proposed 4, 1-benzoxazepin-2-one derivatives of the general formula
where R 1 is a hydrogen atom or an optionally substituted hydrocarbon group; R 2 and R 3 are independently a hydrogen atom, an optionally substituted lower alkyl, an optionally substituted phenyl, or an optionally substituted aromatic heterocyclic group; X is a bond or spacer having a chain length of from 1 to 7 atoms; Y is an optionally esterified or thioetherified carboxyl, optionally substituted hydroxyl, an optionally substituted amino group, an optionally substituted phenyl, an optionally substituted carbamoyl or N-containing heterocyclic residue having a hydrogen atom capable of being deprotonated; with the proviso that when X is methylene and R 1 is not alkyl containing more than 4 carbon atoms, Y is neither carboxyl nor alkoxycarbonyl; ring A may be optionally substituted, or its salts, which are useful for inhibiting squalene synthetase and fungal growth.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP04-099541 | 1992-04-20 | ||
| JP9954192 | 1992-04-20 | ||
| JP33994792 | 1992-12-21 | ||
| JP04-339947 | 1992-12-21 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU99118298/04A Division RU2170732C2 (en) | 1993-04-19 | 1993-04-19 | Derivatives of 4,1-benzoxazepine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU93005332A true RU93005332A (en) | 1996-02-27 |
| RU2145603C1 RU2145603C1 (en) | 2000-02-20 |
Family
ID=26440672
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU93005332/04A RU2145603C1 (en) | 1992-04-20 | 1993-04-19 | Derivatives of 4,1-benzoxazepine, pharmaceutical composition, method of inhibition of activity of squalene synthetase in mammals, method of inhibition of fungi growth in mammals |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP0567026B1 (en) |
| KR (1) | KR100293338B1 (en) |
| CN (1) | CN1044237C (en) |
| AT (1) | ATE235474T1 (en) |
| AU (1) | AU659543B2 (en) |
| CA (1) | CA2094335C (en) |
| DE (1) | DE69332792T2 (en) |
| FI (1) | FI119022B (en) |
| HU (1) | HUT71482A (en) |
| NO (1) | NO304520B1 (en) |
| NZ (1) | NZ247429A (en) |
| RU (1) | RU2145603C1 (en) |
| SG (2) | SG48855A1 (en) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5726306A (en) * | 1992-04-20 | 1998-03-10 | Takeda Chemical Industries, Ltd. | 4,1-benzoxazepin derivatives and their use |
| AU678503B2 (en) * | 1993-09-24 | 1997-05-29 | Takeda Chemical Industries Ltd. | Condensed heterocyclic compounds and their use as squalene synthetase inhibitors |
| WO1995021834A1 (en) * | 1994-02-09 | 1995-08-17 | Takeda Chemical Industries, Ltd. | Optically active 4,1-benzoxazepine derivatives useful as squalene synthase inhibitors |
| JPH10503468A (en) * | 1994-03-24 | 1998-03-31 | メリル・フアーマシユウテイカルズ・インコーポレイテツド | Hypocholesterolemic, antiatherosclerotic and hypotriglyceridemic mercaptoacetylamide disulfide derivatives |
| TW401301B (en) * | 1994-10-07 | 2000-08-11 | Takeda Chemical Industries Ltd | Antihypertriglyceridemic composition |
| EP0710725A1 (en) * | 1994-11-01 | 1996-05-08 | Takeda Chemical Industries, Ltd. | Production of optically active compounds |
| MX9704683A (en) * | 1994-12-23 | 1997-09-30 | Pfizer | Naphthyl-benzoxazepines or -benzothiazepines as squalene synthetase inhibitors. |
| US6110909A (en) * | 1995-09-13 | 2000-08-29 | Takeda Chemical Industries, Ltd. | Benzoxazepine compounds, their production and use as lipid lowering agents |
| CN1072649C (en) * | 1995-09-13 | 2001-10-10 | 武田药品工业株式会社 | Benzoxazepine compounds, their production method and use |
| US6537987B1 (en) * | 1996-06-20 | 2003-03-25 | Pfizer Inc. | 4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors |
| ATE309993T1 (en) | 1997-04-21 | 2005-12-15 | Takeda Pharmaceutical | 4,1-BENZOXAZEPINES, THEIR ANALOGUES, AND THEIR USE AS SOMATOSTATIN AGONISTS |
| JP2001514256A (en) | 1997-09-02 | 2001-09-11 | デュポン ファーマシューティカルズ カンパニー | 5,5-Disubstituted-1,5-dihydro-4,1-benzoxazepin-2 (3H) -ones useful as HIV reverse transcriptase inhibitors |
| US6063921A (en) * | 1997-11-20 | 2000-05-16 | Pharm-Eco Laboratories, Inc. | Synthesis of 11-aryl-5,6-dihydro-11H-dibenz[b,e]azepines |
| US6207664B1 (en) | 1998-11-25 | 2001-03-27 | Pfizer Inc. | Squalene synthetase inhibitor agents |
| PL360243A1 (en) * | 2000-06-23 | 2004-09-06 | Takeda Chemical Industries,Ltd | Benzoxazepinones and their use as squalene synthase inhibitors |
| JO2654B1 (en) | 2000-09-04 | 2012-06-17 | شركة جانسين فارماسوتيكا ان. في | Polyarylcarboxamides useful as lipid lowering agents |
| JO2409B1 (en) | 2000-11-21 | 2007-06-17 | شركة جانسين فارماسوتيكا ان. في | Biphenylcarboxamides useful as lipid lowering agents |
| JO2390B1 (en) | 2001-04-06 | 2007-06-17 | شركة جانسين فارماسوتيكا ان. في | Lipid lowering biphenulcarboxamides |
| CA2451163A1 (en) * | 2001-06-28 | 2003-01-09 | Takeda Chemical Industries, Ltd. | Agent for preventing or treating organ functional disorders and order dysfunction |
| GB0125532D0 (en) * | 2001-10-24 | 2001-12-12 | Burton Michael | Enzyme activity indicators |
| UA79300C2 (en) | 2002-08-12 | 2007-06-11 | Janssen Pharmaceutica Nv | N-aryl piperidine substituted biphenylcarboxamides as inhibitors of apolipoprotein b secretion |
| EP1591120A4 (en) * | 2003-01-28 | 2009-06-10 | Takeda Chemical Industries Ltd | Receptor agonists |
| US7829552B2 (en) | 2003-11-19 | 2010-11-09 | Metabasis Therapeutics, Inc. | Phosphorus-containing thyromimetics |
| US7323455B2 (en) | 2004-03-24 | 2008-01-29 | Wyeth | 7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators |
| JP2009512715A (en) | 2005-10-21 | 2009-03-26 | ノバルティス アクチエンゲゼルシャフト | Combination of renin inhibitor and anti-dyslipidemic agent and / or anti-obesity agent |
| WO2010093601A1 (en) | 2009-02-10 | 2010-08-19 | Metabasis Therapeutics, Inc. | Novel sulfonic acid-containing thyromimetics, and methods for their use |
| US20130156720A1 (en) | 2010-08-27 | 2013-06-20 | Ironwood Pharmaceuticals, Inc. | Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders |
| CN103965185B (en) * | 2014-03-28 | 2016-06-29 | 河北师范大学 | 1,5-benzodiazepine compound containing thiazolyl and ester group and application thereof |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5735596A (en) * | 1980-08-13 | 1982-02-26 | Funai Corp | Ester derivative of deoxyfluorouridine |
| US4374842A (en) * | 1980-04-18 | 1983-02-22 | Shionogi & Co., Ltd. | 4,1-Benzoxazepines and compositions |
| JPS5735576A (en) * | 1980-07-18 | 1982-02-26 | Takeda Chem Ind Ltd | 4,1-benzoxazepin-3-acetic derivative and its production |
| US4590187A (en) * | 1983-11-17 | 1986-05-20 | The Upjohn Company | Phospholipase A2 inhibition using 4,1-benzoxazepine-2-(3H)-ones |
| DE3471101D1 (en) * | 1983-11-17 | 1988-06-16 | Upjohn Co | N-substituted-5-phenyl-4,1-benzoxazepin-2(3h)-ones having therapeutic utility |
| US4758559A (en) * | 1986-01-21 | 1988-07-19 | Ciba-Geigy Corporation | Pyrrolo[1,2-a] [4,1]benzoxazepine derivatives useful as calmodulin and histamine inhibitors |
| NZ239663A (en) * | 1990-09-13 | 1993-07-27 | Merck & Co Inc | Ester derivatives of dioxabicyclo(3,2,1)-octane, medicaments, and a fungus which makes them |
| AU1752792A (en) * | 1991-03-08 | 1992-10-06 | Rhone-Poulenc Rorer International (Holdings) Inc. | Multicyclic tertiary amine polyaromatic squalene synthetase inhibitors |
-
1993
- 1993-04-17 SG SG1996003103A patent/SG48855A1/en unknown
- 1993-04-17 SG SG9903981A patent/SG82630A1/en unknown
- 1993-04-17 DE DE69332792T patent/DE69332792T2/en not_active Expired - Fee Related
- 1993-04-17 AT AT93106276T patent/ATE235474T1/en not_active IP Right Cessation
- 1993-04-17 EP EP93106276A patent/EP0567026B1/en not_active Expired - Lifetime
- 1993-04-19 AU AU37003/93A patent/AU659543B2/en not_active Ceased
- 1993-04-19 RU RU93005332/04A patent/RU2145603C1/en not_active IP Right Cessation
- 1993-04-19 FI FI931763A patent/FI119022B/en active IP Right Grant
- 1993-04-19 NO NO931433A patent/NO304520B1/en unknown
- 1993-04-19 CA CA002094335A patent/CA2094335C/en not_active Expired - Fee Related
- 1993-04-19 NZ NZ247429A patent/NZ247429A/en not_active IP Right Cessation
- 1993-04-20 KR KR1019930006653A patent/KR100293338B1/en not_active IP Right Cessation
- 1993-04-20 CN CN93106358A patent/CN1044237C/en not_active Expired - Fee Related
- 1993-04-20 HU HU9301164A patent/HUT71482A/en unknown
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